2-Fluoroformycin and 2-Aminoformycin. Synthesis and Biological Activity

Article abstract of DOI:10.1021/jm00149a033

Syntheses of 2-fluoroformacin <7-amino-5-fluoro-3-(β-D-ribofuranosyl)pyrazolo<4,3-d>pyrimidine> (2b) and 2-aminoformacin <5,7-diamino-3-(β-D-ribofuranosyl)pyrazolo<4,3-d>pyrimidine> (2c) are described.Cytotoxicity data are given for 2b and 2c alone as well as with added pentostatin.Kinetic parameters for adenosine deaminase are also provided. 2-Fluoroformycin, although a much poorer substrate for adenosine deaminase than formycin A, is not nearly as cytotoxic to cells in culture.